US 3299078A
· Pachter
· 1967
[cited by applicant]
US 3813392A
· Sellstedt
· 1974
[cited by applicant]
US 4001263A
· Plattner et al.
· 1977
[cited by applicant]
US 4238607A
· Rajagopalan
· 1980
[cited by applicant]
US 4389330A
· Tice et al.
· 1983
[cited by applicant]
US 4522944A
· Doria et al.
· 1985
[cited by applicant]
US 4530840A
· Tice et al.
· 1985
[cited by applicant]
US 4767628A
· Hutchinson
· 1988
[cited by applicant]
US 5004602A
· Hutchinson
· 1991
[cited by applicant]
US 5114976A
· Norden
· 1992
[cited by applicant]
US 5151419A
· Perenyi et al.
· 1992
[cited by applicant]
US 5538739A
· Bodmer et al.
· 1996
[cited by applicant]
US 6407092B1
· Hester et al.
· 2002
[cited by applicant]
US 6544559B2
· Mesens et al.
· 2003
[cited by applicant]
US 6548493B1
· Robichaud et al.
· 2003
[cited by applicant]
US 6552017B1
· Robichaud et al.
· 2003
[cited by applicant]
US 6699852B2
· Robichaud et al.
· 2004
[cited by applicant]
US 6713471B1
· Robichaud et al.
· 2004
[cited by applicant]
US 6849619B2
· Robichaud et al.
· 2005
[cited by applicant]
US 6849640B2
· Ennis et al.
· 2005
[cited by applicant]
US 7071186B2
· Robichaud et al.
· 2006
[cited by applicant]
US 7081455B2
· Robichaud et al.
· 2006
[cited by applicant]
US 7109339B2
· Lee et al.
· 2006
[cited by applicant]
US 7183282B2
· Robichaud et al.
· 2007
[cited by applicant]
US RE39679E
· Robichaud et al.
· 2007
[cited by applicant]
US RE39680E
· Robichaud et al.
· 2007
[cited by applicant]
US 7238690B2
· Robichaud et al.
· 2007
[cited by applicant]
US 7375226B2
· Jolidon et al.
· 2008
[cited by applicant]
US 7592454B2
· Lee et al.
· 2009
[cited by applicant]
US 7645752B2
· McDevitt et al.
· 2010
[cited by applicant]
US 8309722B2
· Tomesch et al.
· 2012
[cited by applicant]
US 8598119B2
· Mates et al.
· 2013
[cited by applicant]
US 8648077B2
· Tomesch et al.
· 2014
[cited by applicant]
US 8779139B2
· Tomesch et al.
· 2014
[cited by applicant]
US 8993572B2
· Mates et al.
· 2015
[cited by applicant]
US 9161061B2
· Mesh-Iliescu et al.
· 2015
[cited by applicant]
US 9168258B2
· Mates et al.
· 2015
[cited by applicant]
US 9199995B2
· Tomesch et al.
· 2015
[cited by applicant]
US 9315504B2
· Tomesch et al.
· 2016
[cited by applicant]
US 9371324B2
· Mates et al.
· 2016
[cited by applicant]
US 9393192B2
· Yam et al.
· 2016
[cited by applicant]
US 9428506B2
· Mates et al.
· 2016
[cited by applicant]
US 9586960B2
· Tomesch et al.
· 2017
[cited by applicant]
US 9616061B2
· Mates et al.
· 2017
[cited by applicant]
US 9708322B2
· Li et al.
· 2017
[cited by applicant]
US 9745300B2
· Mates et al.
· 2017
[cited by applicant]
US 9751883B2
· Tomesch et al.
· 2017
[cited by applicant]
US 9956227B2
· Vanover et al.
· 2018
[cited by applicant]
US RE48839E
· Mates et al.
· 2021
[cited by applicant]
US 20040034015A1
· Robichaud et al.
· 2004
[cited by applicant]
US 20040127482A1
· Robichaud et al.
· 2004
[cited by applicant]
US 20110269777A1
· Bachurin et al.
· 2011
[cited by applicant]
US 20200157100A1
· Li
· 2020
[cited by applicant]
US 20200392135A1
· Wennogle et al.
· 2020
[cited by applicant]
US 20200405713A1
· Mates et al.
· 2020
[cited by applicant]
US 20210008065A1
· Li et al.
· 2021
[cited by applicant]
US 20230372336A1
· Dutheil et al.
· 2023
[cited by applicant]
EP 1564671A1
· 2005
[cited by applicant]
WO 2000064899A1
· 2000
[cited by applicant]
WO 2000077001A1
· 2000
[cited by applicant]
WO 2000077002A1
· 2000
[cited by applicant]
WO 2000077010A2
· 2000
[cited by applicant]
WO 2003091250
· 2003
[cited by applicant]
WO 2008112280A1
· 2008
[cited by applicant]
WO 2017117514A1
· 2017
[cited by applicant]
WO 2018031535A1
· 2018
[cited by applicant]
WO 2018106916A1
· 2018
[cited by applicant]
WO 2019102240A1
· 2019
[cited by applicant]
WO 2021119334
· 2021
[cited by applicant]
McIntyre et al., “The Efficacy of Lumateperone in Patients with Bipolar Depression with Mixed Features,” J Clin Psychiatry, vol. 84, No. 3, 10 pages (2023).
[cited by applicant]
McIntyre et al., “The Efficacy of Lumateperone on Symptoms of Depression in Bipolar I and Bipolar II Disorder: Secondary and Post Hoc Analyses,” European Neuropsychopharmacology, vol. 68, p. 78-88, (2023).
[cited by applicant]
Newton, W., “Intra Intra-Cellular Reports Positive Phase III Trial of Caplyta in MDD and Bipolar Depression,” ClinicalTrials Arena, Mar. 29, 2023, retrieved from https://www.clinicaltrialsarena.com/news/news-intra-cellu…
[cited by applicant]
Snyder, G. et al., “Functional Profile of a Novel Modulator of Serotonin, Dopamine, and Glutamate Neurotransmission,” Psychopharmacology, vol. 232, No. 3, 605-621, (2015); Published online Aug. 2014, DOI 10.1007/s00213-…
[cited by applicant]
“Clinical Trial Evaluating ITI-007 (Lumateperone) as a Monotherapy for the Treatment of Bipolar,” ClinicalTrials.gov (Identifier: NCT02600494), 5 pages, (2015).
[cited by applicant]
“Clinical Trial Evaluating ITI-007 as an Adjunctive Therapy to Lithium or Valproate for the Treatment of Bipolar Depression,” ClinicalTrials.gov, 6 pages, Nov. 9, 2015.
[cited by applicant]
“Study of a Novel Antipsychotic ITI-007 in Schizophrenia,” Clinical Trials.gov, 6 pages, Dec. 26, 2011.
[cited by applicant]
Aiken, C., “An Overview of Atypical Antipsychotics for Bipolar Depression,” published on Jan. 3, 2020 at https://www.psychiatrictimes.com/view/overview-atypical-antipsychotics-bipolar-depression, 11 pages.
[cited by applicant]
Barman, R. et al., “Newer Antipsychotics: Brexpiprazole, Cariprazine, and Lumateperone: A Pledge or Another Unkept Promise?,” World J. Psychiatr., vol. 11, No. 12, pp. 1228-1238, (2021).
[cited by applicant]
Bastin, R. et al., “Salt Selection and Optimized Procedures for Pharmaceutical New Chemical Entities,” Organic Process and Research Development, vol. 4, No. 5, pp. 427-435, (2000).
[cited by applicant]
Calabrese, J. et al., “Efficacy and Safety of Lumateperone for Major Depressive Episodes Associated with Bipolar I or Bipolar II Disorder: A Phase 3 Randomized Placebo-Controlled Trial,” American Journal of Psychiatry, …
[cited by applicant]
Correll, C. et al., “Efficacy and Safety of Lumateperone for Treatment of Schizophrenia A Randomized Clinical Trial,” JAMA Psychiatry, vol. 77, No. 4, pp. 349-358, (2020).
[cited by applicant]
Davis, R. et al., “ITI-007 demonstrates brain occupancy at serotonin 5-HT2A and dopamine D2 receptors and serotonin transporters using positron emission tomography in healthy volunteers,” Psychopharmacology, vol. 232, p…
[cited by applicant]
Davis, R. et al., “ITI-007 in the treatment of schizophrenia: from novel pharmacology to clinical outcomes,” Expert Review of Neurotherapeutics, vol. 16, No. 6, pp. 601-614 (2016).
[cited by applicant]
Davis, R. et al., “ITI-007: A Novel Treatment for Behavioral Disturbances Associated with Dementia and Related Disorders,” Clinical Trials in Alzheimer's Disease (CTAD) Congress 2014 (2014) (poster presentation).
[cited by applicant]
Davis, R. et al., “Rationale for the Development of Low Doses of ITI-007 for the Treatment of Behavioral Disturbances Associated with Dementia,” The Journal of Prevention of Alzheimer's Disease, 2(4):302 (2015) (Clinica…
[cited by applicant]
Davis, R. et al., “Lumateperone (ITI-007), A Novel Drug in Development for the Treatment of Agitation in Patients with Dementia, including Alzheimer's Disease: Rationale and Clinical Design,” The Journal of Prevention o…
[cited by applicant]
Edinoff, A. et al., “Lumateperone for the Treatment of Schizophrenia,” Psychopharmacology Bulletin, vol. 50, No. 4, pp. 32-59, (2020).
[cited by applicant]
Gramigna, J, “Lumateperone Safe, Effective for Depressive Symptoms Among Patients with Bipolar Disorders,” American Society of Clinical Psychopharmacology Annual Meeting, Jun. 2, 2020, 3 pages.
[cited by applicant]
Hackam, D. et al., “Translation of Research Evidence from Animals to Humans,” JAMA, vol. 296, No. 14, pp. 1731-1732, (2006).
[cited by applicant]
Harvey, P. et al., “Lumateperone Improves Negative Symptoms Related to Emotional Experience (Avolition) in Patient with Schizophrenia,” Abstract presented at the American Society of Clinical Psychopharmacology (ASCP) An…
[cited by applicant]
Hlavinka, E., “Schizophrenia Tx Eases Depression in Bipolar Disorder: Lumateperone Offers Greater Rate of Response, Remission versus Placebo,” Medpage Today, 7 pages, (2020); https://www.medpagetoday.com/meetingcoverage…
[cited by applicant]
Intra-Cellular Therapies, Inc., “Corporate Presentation” (Sep. 24, 2019), downloaded from https://ir.intracellulartherapies.com/static-files/93b08960-f01c-4864-aa22-8cadb3539753 (last accessed Mar. 13, 2023).
[cited by applicant]
Kantrowitz, J., “The Potential Role of Lumateperone-Something Borrowed? Something New?,” JAMA Psychiatry, vol. 77, No. 4, pp. 343-344, (2020), Abstract only.
[cited by applicant]
Kendrick, T., “The Newer, ‘Atypical’ Antipsychotic Drugs—Their Development and Current Therapeutic Use,” British J. General Practice, vol. 49, pp. 745-749, (1999).
[cited by applicant]
Khorana, N. et al., “Gamma-Carbolines: Binding at 5-HT5A Serotonin Receptors,” Bioorganic & Medicinal Chemistry, vol. 11, D. 717-722, p. 718, Table 1, (2003).
[cited by applicant]
Kumar, B. et al., “Lumateperone: A New Treatment Approach for Neuropsychiatric Disorders,” Drugs of Today, vol. 54, No. 12, pp. 713-719, (2018).
[cited by applicant]
Lammers, L. et al., “Risperidone Long-acting Injection in Schizophrenia Spectrum Illnesses Compared to First Generation Depot Antipsychotics in an Outpatient Setting in Canada,” BMC Psychiatry, vol. 13, No. 155, 9 pages…
[cited by applicant]
Lee, T. et al., “Novel, Highly Potent, Selective 5-HT2A/D2 Receptor Antagonists as Potential Atypical Antipsychotics,” Bioorganic & Medicinal Chemistry Letters, vol. 13, pp. 767-770, (2003).
[cited by applicant]
Li, P. et al., “Discovery of a Tetracyclic Quinoxaline Derivative as a Potent and Orally Active Multifunctional Drug Candidate for the Treatment of Neuropsychiatric and Neurological Disorders,” Journal of Medicinal Chem…
[cited by applicant]
Liebermann, J. et al., “ITI-007 for the Treatment of Schizophrenia: A 4-Week Randomized, Double-Blind, Controlled Trial,” Biological Psychiatry, vol. 79, pp. 952-961, (2016).
[cited by applicant]
Makadia, H. et al., “Poly Lactic-co-Glycolic Acid (PLGA) as Biodegradable Controlled Drug Delivery Carrier,” NIH Public Access, Authors Manuscript, available in PMC 2012, 19 pages, front page states: Published in final …
[cited by applicant]
Marek, G. et al., “Synergistic Action of 5-HT2A Antagonists and Selective Serotonin Reuptake Inhibitors in Neuropsychiatric Disorder,” Neuropsychopharmacology, vol. 28, pp. 402-412, (2003).
[cited by applicant]
McIntyre, R. et al., “Rapid-acting Antidepressants in Psychiatry: Psychedelics, Episodic Treatments, Innovation, and Clarion Call for Methodologic Rigor in Drug Development,” Expert Opinion on Drug Safety, vol. 21, No. …
[cited by applicant]
O'Gorman, et al., “Lumateperone (ITI-007): A Novel Investigational Agent with Broad Therapeutic Potential Across Multiple Neuropsychiatric Disorders,” Poster P.1.g.038, European College of Neuropsychopharmacology (ECNP)…
[cited by applicant]
Press Release, “Intra-Cellular Therapies Announces Additional Results From Phase I/II Clinical Trial for ITI-007 in Healthy Geriatric Subjects and Patients With Dementia,” Intra-Cellular Therapies, Press Release Date: N…
[cited by applicant]
Press Release, “Intra-Cellular Therapies Announces Positive Top-Line Results from a Phase 3 Trial of Lumateperone in Patient with Bipolar Depression,” Intra-Cellular Therapies, Press Release Date: Jul. 8, 2019.
[cited by applicant]
Press Release, “Intra-Cellular Therapies Announces Top-Line Results from the Second Phase 3 Trial of ITI-007 in Patients with Schizophrenia (Study '302)”, Intra-Cellular Therapies, Press Release Date: Sep. 28, 2016, 8 p…
[cited by applicant]
Press Release, “Intra-Cellular Therapies Presents Data on Symptom Improvement by Lumateperone on Negative Symptoms, Depression, and Social Function in Patients with Schizophrenia at the American Society of Clinical Psyc…
[cited by applicant]
Press Release, “Intra-Cellular Therapies Reports Positive Final Results of a Phase II Clinical Trial With ITI-007 in Patients with Sleep Maintenance Insomnia.”, Intra-Cellular Therapies, Press Release Date: Mar. 10, 200…
[cited by applicant]
Pubchem, OPEN Chemistry Database, PubChem SID 103920954, PubChem CID 90655118, (2011), 6 pages.
[cited by applicant]
Rainer, M., “Risperidone Long-acting Injection: A Review of its Long Term Safety and Efficacy,” Neuropsychiatric Disease and Treatment, vol. 4, No. 5, pp. 919-927, (2008).
[cited by applicant]
Satlin, A. et al., “ITI-007 (Lumateperone) for the Treatment of Agitation in Patients with Dementia, including Alzheimer's Disease,” Alzheimer's & Dementia, vol. 14, No. 7, pp. 678-679, (2018), (Alzheimer's Assoc. Inter…
[cited by applicant]
Satlin, A. et al., “ITI-007 (Lumateperone) for the Treatment of Agitation in Patients with Dementia, including Alzheimer's Disease,” Poster P2-032, Alzheimer's Assoc. International Conference 2018, (2018).
[cited by applicant]
Tohen, M. et al., “Efficacy of Olanzapine and Olanzapine-Fluoxetine Combination in the Treatment of Bipolar I Depression,” Arch Gen Psychiatry, vol. 60, pp. 1079-1088, (2003).
[cited by applicant]
Vanover, K. et al., “Dopamine D2 receptor occupancy of lumateperone (ITI-007): a Positron Emission Tomography Study in patients with schizophrenia,” Neuropsychopharmacology, vol. 44, pp. 598-605, (2019).
[cited by applicant]
Vanover, K. et al., “ITI-007: A Novel Therapy for the Treatment of Schizophrenia and Related Psychoses,” International Clinical Psychopharamcology, vol. 26, e56, 1 page, (2011).
[cited by applicant]
Vanover, K. et al., “A Novel Approach to Address an Unmet Need in the Treatment of Schizophrenia and Depression: Lumateperone, an Innovative Modulator of Dopamine, Serotonin, and Glutamate,” Abstract presented at the Am…
[cited by applicant]
Vanover, K. et al., “Lumateperone (ITI-007): A Novel Investigational Agent with Broad Therapeutic Potential Across Multiple Neuropsychiatric Disorders,” European Neuropsychopharmacology, vol. 27, pp. S660-S661 (2017) (S…
[cited by applicant]
Vanover, K. et al., Abstracts of the 13th International Congress on Schizophrenia (ICOSR) (Apr. 2-6, 2011), Schizophrenia Bull., vol. 37, Suppl. 1., p. 325, (2011).
[cited by applicant]
Vyas, P. et al., “An Evaluation of Lumateperone Tosylate for the Treatment of Schizophrenia,” Expert Opinion on Pharmacotherapy, vol. 21, No. 2, pp. 139-145, (2020); https://doi.org/10.1080/14656566.2019.1695778.
[cited by applicant]
Wang, S. et al., “Rapid-acting Antidepressants Targeting Modulation of the Glutamatergic System: Clinical and Preclinical Evidence and Mechanisms,” General Psychiatry, vol. 35, No. e100922, 6 pages, (2022).
[cited by applicant]
Wennogle, L. et al., “Activation of NMDA and AMPA Receptors by Lumateperone (ITI-007): Implications for Antidepressant Activity,” Abstract presented at the 2017 Collegium Internationale Neuro-Psychopharmacologicum (CINP…
[cited by applicant]
Witkin, J. et al., “Chapter 3: Rapid-acting Antidepressants,” Advances in Pharmacology, vol. 86, 50 pages, (2019).
[cited by applicant]
“Guidance for Industry: Q3A Impurities in New Drug Substances,” U.S. Food & Drug Administration, Center for Drug Evaluation and Research, Jun. 2008 (last accessed Apr. 3, 2025) (available at https://www.fda.gov/media/71…
[cited by applicant]
Defendants' Joint Initial Invalidity Contentions, Ex. E ('419 Patent),
[cited by applicant]
Defendants' Joint Initial Invalidity Contentions, Ex. P ('792 Patent),
[cited by applicant]
Hofmann et al., “Effect of Treatments for Depression on Quality of Life: A Meta-Analysis,” Cogn. Behav. Ther., vol. 46, No. 4, p. 265-286, (2017).
[cited by applicant]
Press Release, “Intra-Cellular Therapies, Inc. Receives Exclusive License for Central Nervous System Compounds from Bristol-Myers Squibb Company,” Intra-Cellular Therapies, Inc. Press Release Date: Jun. 1, 2005.
[cited by applicant]